Literature DB >> 28495080

Determine equilibrium dissociation constant of drug-membrane receptor affinity using the cell membrane chromatography relative standard method.

Weina Ma1, Liu Yang1, Yanni Lv1, Jia Fu1, Yanmin Zhang1, Langchong He2.   

Abstract

The equilibrium dissociation constant (KD) of drug-membrane receptor affinity is the basic parameter that reflects the strength of interaction. The cell membrane chromatography (CMC) method is an effective technique to study the characteristics of drug-membrane receptor affinity. In this study, the KD value of CMC relative standard method for the determination of drug-membrane receptor affinity was established to analyze the relative KD values of drugs binding to the membrane receptors (Epidermal growth factor receptor and angiotensin II receptor). The KD values obtained by the CMC relative standard method had a strong correlation with those obtained by the frontal analysis method. Additionally, the KD values obtained by CMC relative standard method correlated with pharmacological activity of the drug being evaluated. The CMC relative standard method is a convenient and effective method to evaluate drug-membrane receptor affinity.
Copyright © 2017 Elsevier B.V. All rights reserved.

Keywords:  Cell membrane chromatography; Drug-membrane receptor affinity; Equilibrium dissociation constant; Relative standard method

Mesh:

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Year:  2017        PMID: 28495080     DOI: 10.1016/j.chroma.2017.04.053

Source DB:  PubMed          Journal:  J Chromatogr A        ISSN: 0021-9673            Impact factor:   4.759


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